ofatumumab Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
human origin 4951 679818-59-8

Description:

MoleculeDescription

Synonyms:

  • ofatumumab
  • arzerra
  • GSK1841157
  • HuMax-CD20
  • 2F2
Ofatumumab is a human monoclonal antibody (IgG1) that binds specifically to a distinct epitope encompassing both the small and large extracellular loops of the CD20 molecule. The CD20 molecule is a transmembrane phosphoprotein expressed on B lymphocytes from the pre-B to mature B lymphocyte stage and on B cell tumours. The binding of ofatumumab to the membrane-proximal epitope of the CD20 molecule induces recruitment and activation of the complement pathway at the cell surface, leading to complement dependent cytotoxicity and resultant lysis of tumour cells. Ofatumumab has been shown to induce appreciable lysis of cells with high expression levels of complement defence molecules.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 23, 2021 PMDA Novartis Pharma K.K.
April 19, 2010 EMA Novartis Europharm Ltd
Oct. 26, 2009 FDA GLAXO GRP LTD

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 158.86 25.73 86 2652 104850 53241478
Chills 115.74 25.73 70 2668 104778 53241550
Pyrexia 111.66 25.73 119 2619 403074 52943254
Influenza like illness 65.37 25.73 40 2698 60819 53285509
Progressive multifocal leukoencephalopathy 60.73 25.73 23 2715 12106 53334222
Chronic lymphocytic leukaemia 48.81 25.73 14 2724 3102 53343226
Headache 43.61 25.73 89 2649 536732 52809596
Neutropenic sepsis 36.81 25.73 17 2721 14632 53331696
Pneumonia 35.97 25.73 70 2668 407099 52939229
Accidental exposure to product 34.52 25.73 19 2719 23655 53322673
Fatigue 28.63 25.73 92 2646 730414 52615914
Multiple sclerosis relapse 27.79 25.73 21 2717 44832 53301496
Hemianopia 27.72 25.73 7 2731 957 53345371

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 204.64 29.04 132 2979 119434 32390981
Pneumonia 145.68 29.04 173 2938 355079 32155336
Neutropenic sepsis 108.28 29.04 42 3069 12657 32497758
Chronic lymphocytic leukaemia 108.12 29.04 33 3078 4852 32505563
Pyrexia 93.19 29.04 132 2979 319836 32190579
Second primary malignancy 52.26 29.04 21 3090 6920 32503495
Infusion related reaction 50.98 29.04 39 3072 45560 32464855
Disease progression 50.13 29.04 51 3060 86811 32423604
Tumour lysis syndrome 42.98 29.04 23 3088 14524 32495891
Neutropenia 40.03 29.04 58 3053 142117 32368298
Injection related reaction 38.45 29.04 7 3104 104 32510311
Chills 33.08 29.04 39 3072 78045 32432370
Hypercalcaemia 32.91 29.04 19 3092 13875 32496540
Lower respiratory tract infection 30.45 29.04 24 3087 29219 32481196
Sepsis 29.91 29.04 54 3057 158780 32351635

Pharmacologic Action:

SourceCodeDescription
ATC L01FA02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
CD20 (Clusters of Differentiation 20) inhibitors
ATC L04AA52 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA MoA N0000175078 CD20-directed Antibody Interactions
MeSH PA D000970 Antineoplastic Agents
FDA EPC N0000175657 CD20-directed Cytolytic Antibody

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic lymphoid leukemia, disease indication 92814006
Relapsing multiple sclerosis indication 230372003
Secondary progressive multiple sclerosis indication 425500002 DOID:0050783

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
B-lymphocyte antigen CD20 Surface antigen ANTIBODY BINDING Kd 9.92 IUPHAR DRUG LABEL

External reference:

IDSource
D09314 KEGG_DRUG
4029460 VUID
N0000180305 NUI
4029460 VANDF
CHEMBL1201836 ChEMBL_ID
C527517 MESH_SUPPLEMENTAL_RECORD_UI
6778 IUPHAR_LIGAND_ID
8606 INN_ID
DB06650 DRUGBANK_ID
M95KG522R0 UNII
8254 PUBCHEM_CID
712566 RXNORM
168892 MMSL
26825 MMSL
d07509 MMSL
013301 NDDF
444607009 SNOMEDCT_US
444609007 SNOMEDCT_US
895672000 SNOMEDCT_US
C1832027 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ARZERRA HUMAN PRESCRIPTION DRUG LABEL 1 0078-0669 INJECTION, SOLUTION 20 mg INTRAVENOUS BLA 26 sections
ARZERRA HUMAN PRESCRIPTION DRUG LABEL 1 0078-0690 INJECTION, SOLUTION 20 mg INTRAVENOUS BLA 26 sections
KESIMPTA HUMAN PRESCRIPTION DRUG LABEL 1 0078-1007 INJECTION, SOLUTION 20 mg SUBCUTANEOUS BLA 30 sections